This study will be a single-center, phase I, randomized, open, in fed condition, parallel, single dose study to evaluate the pharmacokinetics and the safety, tolerability of Atovaquone/proguanil combination tablets and atovaquone suspension in Japanese healthy male subjects. Serial blood samples will be collected for the determination of the plasma concentration of atovaquone, proguanil and cycloguanil after dosing of atovaquone 1000mg/proguanil 400 mg and the plasma atovaquone concentration of atovaquone 750 and 1500 mg. Safety assessments will be performed for each treatment group. CYP2C19 contribute to proguanil metabolism. CYP2C19 genotype will be determined in atovaquone/proguanil dosing group.
Study Type
INTERVENTIONAL
Allocation
RANDOMIZED
Purpose
OTHER
Masking
NONE
Enrollment
30
Atovaquone/proguanil HCL
Atovaquone
GSK Investigational Site
Kagoshima, Japan
plasma atovaquone concentration
Time frame: pre, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 120, 168, 216, 336 post dose
plasma proguanil concentration
Time frame: pre, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 120, 168, 216, 336 post dose
plasma cycloguanil concentration
Time frame: pre, 1, 2, 3, 4, 6, 8, 10, 12, 16, 24, 48, 72, 120, 168, 216, 336 post dose
Number of participants with adverse events
Time frame: up to 336h post dose
Change in Systolic Blood Pressure
Change values at 4, 24, 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 4, 24, 72, 168 and 336 h post-dose
Change in ECG findings
Change at 4, 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 4, 72, 168 and 336 h post-dose
Laboratory
Change values at 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 72, 168 and 336 h post-dose
Change in Diastolic Blood Pressure
Change values at 4, 24, 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 4, 24, 72, 168 and 336 h post-dose
Change in Heart rate
Change values at 4, 24, 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 4, 24, 72, 168 and 336 h post-dose
Change in Hematology values
Change values at 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 72, 168 and 336 h post-dose
Change in Biochemistry values
Change values at 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 72, 168 and 336 h post-dose
Change in Urinalysis values
Change values at 72, 168 and 336 h post-dose from baseline (pre-dose)
Time frame: at pre-dose, 72, 168 and 336 h post-dose
This platform is for informational purposes only and does not constitute medical advice. Always consult a qualified healthcare professional.